Abstract
1. We have previously shown that weaning at day 21 increases delta-opioid receptor binding in the brain at day 25, which might be due to stimulation of the development of a delta-opioid receptor subtype or activation of G-protein coupling processes. 2. We have addressed the possibility that weaning stimulates coupling of the delta-receptor by homogenate binding studies with four agonist and one antagonist radioligand in the presence of a GTP analogue and Na+ in brain tissue from weaned and non-weaned animals. 3. Saturation studies with three agonist ligands ([3H]-deltorphin I, [3H]-S-Atc-Ile(5,6)deltorphin I and [3H]-R-Atc-Ile(5,6)deltorphin II) showed higher levels of maximal binding in brains from 25-day weaned than in brains from non-weaned rats. The magnitude of the effects of GMPPNP and Na+ in decreasing this binding was ligand dependent and in each case was significantly more marked in brains from weaned animals. GMPPNP and Na+ were completely without effect on Bmax for, [3H]-S-Atc-Ile(5,6)deltorphin I and [3H]-R-Atc-Ile(5,6)deltorphin II in brains from non-weaned rats. 4. [3H]-Ile(5,6)deltorphin II and [3H]-naltrindole showed no differences in labelling between weaned and non-weaned groups and both groups responded similarly to the effects of GMPPNP and Na+ treatment. 5. GMPPNP and Na+ had small effects on binding affinity (K(D)) for some of the agonist radioligands which were similar in both weaned and non-weaned groups. 6. Weaning induced increases in binding of delta-receptors in 25-day rats can be explained in terms of the way delta-agonist radioligands recognize the receptor environment.